Controlled-release colon targeting drug administration preparation and preparation method thereof

Abstract

The invention relates to a controlled-release colon targeting drug adminitration preparation. The forms of the preparation are colon site-specific coated tablets or colon targeting pellets. The preparation consists of a tablet core or pellet core, an isolating layer and a controlled-release coating layer, wherein the controlled-release coating layer comprises an internal coating layer and an external coating layer. By adopting the multilayer coating technology, enteric soluble acrylic resin water dispersion and osmotic acrylic resin water dispersion are used as main coating materials for carrying out coating, thereby obtaining the controlled-release colon targeting drug adminitration preparation. The preparation of the invention enables drugs to be released at a constant rate at a colon section, realizes accurate site-specific drug release, increases the concentration of the drugs at some parts of positions with pathological changes, is beneficial to treating ulcerative colitis and carcinoma of colon, avoids the stimulation of the drugs on stomaches and small intestines, achieves the goal of colon site-specific drug release, enhances the targeting site-specific curative effect on colon diseases and reduces the toxic and side effect. Compared with the common oral preparations, under the condition of the same drug adminitration dosage, the preparation of the invention can enhance the curative effect and reduce the incidence rate of untoward reactions. Compared with the enemas or the rectal suppositories, the preparation has the advantages of uniform drug distribution in the colon and good patient compliance.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to a novel pH-dependent-time-controlled colon-targeted drug delivery preparation, in particular to a method for preparing a double-coated colon-positioned controlled-release tablet, which is used for the preparation of therapeutic Preparation of acute and chronic ulcerative colitis or colon cancer drugs. Background technique [0002] The colon is a frequent site of digestive tract diseases, and ulcerative colitis (ulcerative colitis, UC) and colon cancer are common intestinal diseases. Ulcerative colitis is an inflammatory and ulcerative lesion of the large intestine mucosa of unknown etiology, mainly involving the rectal mucosa and sigmoid colon mucosa, with continuous non-segmental distribution, even the entire colon and terminal ileum. Clinical manifestations include abdominal pain, diarrhea, mucus, pus and blood in the stool, and tenesmus. The acute fulminant...

AI Technical Summary

Problems solved by technology

Traditional oral administration preparations (such as tablets, capsules, etc.) disintegrate in the stomach after oral administration, and the drug is greatly affected by the contents of the stomach and pH. As well as the destruction of various digestive enzymes, there are very few prototype drugs that reach the colon and take effect

Ordinary enteric-coated preparations are mainly released in the small intestine, and most of the drugs are absorbed into the blood through the small intestine, and the drug metabolism is inactivated due to the destruction of various digestive enzymes in the small intestine and the first-pass effect, which will reduce the concentration of the drug reaching the colon. Unsatisfactory treatment effect

Moreover, common oral preparations and injections are administered, and the toxic and side effects are obvious due to the systemic effect of the drug.

Enema administration or rectal suppository administration has great individual differences, and the distribution of the drug in the colon is uneven, and the drug reaches only the rectum, sigmoid colon, and descending colon, and does not reach the transverse colon and ascending colon, and is inconvenient to use. Heavy workload for medical staff and poor patient compliance

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